Patent EP1131344, entitled 'retro-inversion peptides that target gastro-intestinal tract transport receptors and related methods', covers Merrion's Gastrointestinal Permeation Enhancement Technology (GIPET) technology, designed to allow large molecules such as proteins to be given orally rather than by injection.
GIPET is based on the focused application of proprietary penetration enhancers, which improve the uptake of such drugs in the small intestine. The technology comprises three distinct types of penetration enhancers which are applicable to both solid and liquid-fill dosage forms.
These formulations do not require chemical modification of the active drug, which removes a regulatory barrier to their use in improving existing products, and studies have shown that the penetration enhancing effects are rapidly reversible. The GIPET technologies are applicable to small molecules, macromolecules and biologics, and two of them have Generally Recognised As Safe (GRAS) status in the US.
Merrion, which has its headquarters in the US but still operates its research functions from Ireland, said that the targeting peptides covered under this latest patent have been successfully used to deliver insulin orally in animals.
"This patent is significant in that it provides another approach in our platform of technologies for the oral delivery of problematic drugs," said Thomas Leonard, Merrion's chief scientific officer.
He said the technology provides new opportunities for site selective drug targeting to specific organs and tissues, and can be applied to active drug moieties with a variety of physical-chemical properties.
Merrion said last year that it had already advanced four drugs based on GIPET or its Gastrointestinal Retentions system (GIRES) for drugs with short half-lives into Phase I clinical trials.